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使用富含 DMSO 的大气层进行 HTS 图书馆板的再生

Fraser Hughes¹, Alex Cookson¹, Fabio Tamaki¹

¹Drug Discovery Unit, School of Life Sciences, University of Dundee, DD1 5EH, United Kingdom.

SLAS technology

|October 13, 2024

概括

高通量选 (HTS) 复合库吸收大气中的水分,影响数据的可复制性. 使用干燥二甲基硫氧化物 (DMSO) 环境的新方法消除了这种水合,提高了测试可靠性和节省成本.

科学领域:

药物发现和开发药物发现和开发
化学生物学化学生物学
高通量选 (HTS) 是一种高通量选.

背景情况:

甲基二硫氧化物 (DMSO) 是湿透的,很容易吸收大气中的水分.
在HTS中化合物库的水化导致可变的溶液体积和度.
这种变异性会对生物测试数据的可重复性产生负面影响.

研究的目的:

为了证明样本库水化对生物数据可复制性的有害影响.
介绍一种用于从HTS图书馆板中去除大气水分的新方法.
提高HTS活动中生成的数据的可靠性和质量.

主要方法:

使用无水DMSO在净化储存中创建了一个富含DMSO的环境.
在这个环境中化HTS库板长达3天.
使用蒸发光散射检测 (ELSD) 量化取水及其对化合物度的影响.

主要成果:

脱水显著增加了溶液的度,特别是在不容易溶解的化合物中.
复原的抑制活性 (pIC50) 含有~30%的水的原始溶液,从>30μM到亚微分子.
在HTS中证明了测试化合物的可靠性提高.

结论:

这种新的方法有效地消除了HTS化合物库中的水分.
改善的化合物度和恢复的生物活性提高了试验可靠性.
这种方法可以大大节省成本,并提高药物查中的数据质量.

关键词:

复合管理是一种复合管理.复合存储是一种复合存储.这就是DMSO.高吞吐量选 (HTS) 是指高吞吐量的选.惰性大气层储存.可溶性溶解度溶解度溶解度

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